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Purpose <p>Antimicrobial resistance (AMR) associated with sexually transmitted infections (STIs) is a serious public health concern that has resulted in the failure of available treatment options and necessitated the use of innovative drug delivery platforms. Herein, linezolid (LzD)-infused sol-gels have been prepared for intravaginal drug delivery in drug-resistant STIs.</p> Methods <p>Sol-gel formulations were prepared using poloxamer 407 (P407), poloxamer 188 (P188), hydroxypropyl methyl cellulose E4M (HPMC E4M), and methyl paraben (MP) in citrate buffer (CB). The rheomechanical properties, in vitro drug release, and stability of optimised sol-gels were investigated. Further, ex vivo bovine vaginal tissue permeation and tissue deposition, HeLa-cell-based toxicity evaluation, and antimicrobial screening against methicillin-sensitive and methicillin- and oxacillin-resistant <i>Staphylococcus aureus (S. aureus)</i> were carried out with the lead sol-gel.</p> Results <p>The sol-gels demonstrated a gelation temperature (T<sub>sol-gel</sub>) of 26–28&#xa0;°C, an osmolality &lt; 1200 mOsm/kg, and a pH of ~ 4.0, while displaying a sustained in vitro drug release (54–59 % release at 72&#xa0;h). LzD and rheological stability was maintained during the study period. The lead sol-gel (F10) displayed low tissue permeability (~4.5%) and favourable tissue deposition (202.55 ± 9.50&#xa0;µg/g) at 6&#xa0;h, HeLa cell compatibility, and notable antimicrobial activity against both methicillin- and oxacillin-resistant strains of <i>Staphylococcus aureus (S. aureus).</i></p> Conclusion <p>These studies demonstrate that the sol-gel platform has immense potential for managing drug-resistant STIs, with a low risk of AMR due to localised drug delivery, minimal systemic exposure, dose reduction (<i>c.f.</i> oral delivery), and increased patient compliance.</p>

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Intravaginal application of linezolid-infused sol-gel for prophylaxis and treatment of sexually transmitted infections

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月21日

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  • Ritu Thapa,
  • Preeti Pandey,
  • Marie-Odile Parat,
  • Shila Gurung,
  • Harendra S. Parekh

摘要

Purpose

Antimicrobial resistance (AMR) associated with sexually transmitted infections (STIs) is a serious public health concern that has resulted in the failure of available treatment options and necessitated the use of innovative drug delivery platforms. Herein, linezolid (LzD)-infused sol-gels have been prepared for intravaginal drug delivery in drug-resistant STIs.

Methods

Sol-gel formulations were prepared using poloxamer 407 (P407), poloxamer 188 (P188), hydroxypropyl methyl cellulose E4M (HPMC E4M), and methyl paraben (MP) in citrate buffer (CB). The rheomechanical properties, in vitro drug release, and stability of optimised sol-gels were investigated. Further, ex vivo bovine vaginal tissue permeation and tissue deposition, HeLa-cell-based toxicity evaluation, and antimicrobial screening against methicillin-sensitive and methicillin- and oxacillin-resistant Staphylococcus aureus (S. aureus) were carried out with the lead sol-gel.

Results

The sol-gels demonstrated a gelation temperature (Tsol-gel) of 26–28 °C, an osmolality < 1200 mOsm/kg, and a pH of ~ 4.0, while displaying a sustained in vitro drug release (54–59 % release at 72 h). LzD and rheological stability was maintained during the study period. The lead sol-gel (F10) displayed low tissue permeability (~4.5%) and favourable tissue deposition (202.55 ± 9.50 µg/g) at 6 h, HeLa cell compatibility, and notable antimicrobial activity against both methicillin- and oxacillin-resistant strains of Staphylococcus aureus (S. aureus).

Conclusion

These studies demonstrate that the sol-gel platform has immense potential for managing drug-resistant STIs, with a low risk of AMR due to localised drug delivery, minimal systemic exposure, dose reduction (c.f. oral delivery), and increased patient compliance.